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Biomolecule conjugation strategy using novel water-soluble phosphine-based chelating agents

United States Patent

6,780,397
August 24, 2004
View the Complete Patent at the US Patent & Trademark Office
This invention describes a novel strategy to produce phosphine-functionalized biomolecules (e.g. peptides or proteins) for potential use in the design and development of site-specific radiopharmaceuticals for diagnosis or therapy of specific cancers. Hydrophilic alkyl phosphines, in general, tend to be oxidatively unstable. Therefore, incorporation of such phosphine functionalities on peptide (and other biomolecule) backbones, without oxidizing the P.sup.III centers, is difficult. In this context this discovery reports on a new technology by which phosphines, in the form of bifunctional chelating agents, can be directly incorporated on biomolecular backbones using manual synthetic or solid phase peptide synthesis methodologies. The superior ligating abilities of phosphine ligands, with various diagnostically (e.g. TC-99m) or therapeutically (e.g. Re186/188, Rh-105, Au-199) useful radiometals, coupled with the findings that the resulting complexes demonstrate high in vivo stability makes this approach useful in the development of radiolabeled biomolecules for applications in the design of tumor-specific radiopharmaceuticals.
Katti; Kattesh V. (Columbia, MO), Gali; Hariprasad (Columbia, MO), Volkert; Wynn A. (Columbia, MO)
Curators of the University of Missouri (Columbia, MO)
09/ 386,657
20040042963
August 31, 1999
GRANT INFORMATION Research in this application was supported in part by a grant from the Department of Energy (DEFG0289ER60875). The government has certain rights in the invention.